Global Patent Index - EP 2498759 B1

EP 2498759 B1 20180801 - IMMEDIATE RELEASE TABLET FORMULATIONS

Title (en)

IMMEDIATE RELEASE TABLET FORMULATIONS

Title (de)

TABLETTENFORMULIERUNGEN MIT SOFORTIGER FREISETZUNG

Title (fr)

FORMULATIONS POUR COMPRIMÉS À LIBÉRATION IMMÉDIATE

Publication

EP 2498759 B1 20180801 (EN)

Application

EP 10782116 A 20101112

Priority

  • US 26117309 P 20091113
  • US 2010056577 W 20101112

Abstract (en)

[origin: WO2011060290A2] The present invention provides an immediate release pharmaceutical formulation which includes a tablet or capsule formulation comprising metformin and the sodium dependent glucose transporter (SGLT2) inhibitor dapagliflozin or its propylene glycol hydrate. The present invention also provides methods of preparing the formulations and methods of treating diseases or disorders associated with SGLT2 activity employing these formulations.

IPC 8 full level

A61K 9/20 (2006.01); A61K 31/155 (2006.01); A61K 31/351 (2006.01); A61K 45/06 (2006.01)

CPC (source: EP US)

A61K 9/2054 (2013.01 - EP US); A61K 31/155 (2013.01 - EP US); A61K 31/351 (2013.01 - US); A61K 31/70 (2013.01 - EP US); A61K 45/06 (2013.01 - EP US); A61P 3/04 (2017.12 - EP); A61P 3/06 (2017.12 - EP); A61P 3/10 (2017.12 - EP); A61P 5/50 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 9/10 (2017.12 - EP); A61P 9/12 (2017.12 - EP); A61P 13/12 (2017.12 - EP); A61P 17/02 (2017.12 - EP); A61P 25/00 (2017.12 - EP); A61P 27/02 (2017.12 - EP); A61P 27/12 (2017.12 - EP); A61P 43/00 (2017.12 - EP); A61K 9/209 (2013.01 - EP US)

C-Set (source: EP US)

  1. A61K 31/155 + A61K 2300/00
  2. A61K 31/70 + A61K 2300/00

Citation (opposition)

Opponent : Galenicum Health

  • WO 2008116179 A1 20080925 - BRISTOL MYERS SQUIBB [US], et al
  • EP 2498759 A2 20120919 - BRISTOL MYERS SQUIBB CO [US], et al
  • "View of NCT01002807 on 2009_10_26", CLINICALTRIALS.GOV, 29 July 2015 (2015-07-29), pages 1 - 3, XP002663638
  • PARIKH M DILIP: "Handbook of Pharmaceutical Granulation Technology", 2005, article "6.2.3. Process Related Variables", pages: 269,274 - 277, XP055591597
  • "Handbook of Pharmaceutical Excipients", 2006, article "Cellulose, Microcrystalline", pages: 132 - 135, XP002483911
  • "Handbook of Pharmaceutical Excipients", 2006, article "Hydroxypropyl Cellulose", pages: 336 - 340, XP008167868
  • "Handbook of Pharmaceutical Excipients", 2006, article "Sodium Starch Glycolate", pages: 701 - 704, XP002694443
  • "Handbook of Pharmaceutical Excipients", 2006, article "Hydroxypropyl Cellulose, Low-substituted", pages: 341 - 343, XP002547079
  • "Handbook of Pharmaceutical Excipients", 2005, article "Magnesium Stearate", pages: 430 - 433, XP055591638
  • LIEBERMAN ET AL.: "Pharmaceutical dosage forms: tablets", vol. 1, 1989, article "Bandelin B. Binders", pages: 160, XP055591642
  • "Pharmaceutical dosage forms: tablets", vol. 1, 1989, article "bandelin A. Fillers", pages: 152 - 153, XP055591650
  • "Pharmaceutical dosage forms: tablets", vol. 1, 1989, article "Compressed Tablets by Wet Granulation C. Lubricants", pages: 169, XP055591661
  • "Pharmaceutical dosage forms: tablets volume 1", vol. 1, 1989, article "Compressed Tablets by Wet Granulation D. Disintegrants", pages: 173 - 177, XP055591670
  • "Annex 5 Guidelines for registration of fixed-dose combination medicinal products", WHO TECHNICAL REPORT SERIES NO. 929, 2005, pages 94, 112, XP055591673
  • "GLUCOVANCE® (Glyburide and Metformin HCI Tablets)1.25 mg/250 mg 2.5 mg/500 mg 5 mg/500 mg", 30 September 2006 (2006-09-30), pages 32pp, XP055591676
  • GLAXOSMITHKLINE: "AvandametTM brand of rosiglitazone maleate and metformin hydrochloride tablets", 10 April 2003 (2003-04-10), pages 3 - 22, XP055591704
  • BRISTOL-MYERS SQUIBB: "MetaglipTM (glipizide and metformin HCI) Tablets 2.5 mg/250 mg 2.5 mg/500 mg 5 . mg/500 mg", 18 June 2007 (2007-06-18), pages 1 - 33, XP055591740, Retrieved from the Internet <URL:https://www.accessdata.fda.qov/scripts/cder/daf/index.cfm?event=overview.proce ss&AppINo=021460>
  • "ACTOPLUS MET™ (pioglitazone hydrochloride and metformin hydrochloride tablets)", August 2006 (2006-08-01), pages 27pp, XP055591742
  • "Janumet (sitagliptin and metformin HCI)", January 2008 (2008-01-01), pages 1 - 22, XP055591796
  • "Prandimet® (repaglinide and metformin HCI) Tablets", May 2010 (2010-05-01), pages 1 - 15, XP055591797
  • "Assessment Report for Janumet (EMEA/H/C/000861)", EMEA, 2008, pages 1 - 43, XP055591802

Opponent : Generics (U.K.) Limited

  • US 7589193 B2 20090915 - WASHBURN WILLIAM [US], et al
  • WO 2008116179 A1 20080925 - BRISTOL MYERS SQUIBB [US], et al
  • WO 2011006029 A1 20110113 - UNIV PITTSBURGH [US], et al
  • US 26117309 P 20091113
  • WO 2007131930 A1 20071122 - BOEHRINGER INGELHEIM INT [DE], et al
  • C. J. BAILEY ET AL.: "Fixed-dose single tablet antidiabetic combinations, review article", DIABETES, OBESITY AND METABOLISM, vol. 11, 2009, pages 527 - 533, XP055588773
  • S. A. JABBOUR ET AL.: "Sodium glucose co-transporter 2 inhibitors: blocking renal tubular reabsorption of glucose to improve glycaemic control in patients with diabetes, review article", INT. J. CLIN. PRACTICE, vol. 62, no. 8, 2008, pages 1279 - 1284, XP055402102
  • C. J. BAILEY ET AL.: "Dapagliflozin as an add- on to metformin lowers hyperglycaemia in type 2 diabetes patients inadequately controlled with metformin alone; abstract 169 of oral presentation 29 Novel therapies for type 2 diabetes mellitus at the 45th EASD Annual Meeting of the European Association for the Study of Diab", DIABETOLOGIA, vol. 52, 2009, Vienna, Austria, pages S76
  • "Formulation and Analytical Development for low-dose oral drug products", 2009, Hoboken, New Jersey, article J. ZHENG

Opponent : Hoefer & Partner Patentanwälte mbB

  • WO 2008116179 A1 20080925 - BRISTOL MYERS SQUIBB [US], et al
  • US 2005266080 A1 20051201 - DESAI DIVYAKANT S [US], et al
  • WO 2005117841 A1 20051215 - BRISTOL MYERS SQUIBB CO [US], et al
  • WO 2008113000 A1 20080918 - NECTID INC [US], et al
  • WO 2007078726 A2 20070712 - MERCK & CO INC [US], et al
  • WO 2009011451 A1 20090122 - TAKEDA PHARMACEUTICAL [JP], et al
  • WO 2009099734 A1 20090813 - MERCK & CO INC [US], et al
  • WO 2009111200 A1 20090911 - MERCK & CO INC [US], et al
  • WO 2009121945 A2 20091008 - BOEHRINGER INGELHEIM INT [DE], et al
  • WO 2009143021 A1 20091126 - BRISTOL MYERS SQUIBB CO [US], et al
  • US 2006057202 A1 20060316 - ANTARKAR AMIT K [IN], et al
  • US 2008234366 A1 20080925 - BINDRA DILBIR S [US], et al
  • WO 2010045656 A2 20100422 - NECTID INC [US], et al
  • WO 2010138535 A1 20101202 - BRISTOL MYERS SQUIBB CO [US], et al
  • WO 2011039337 A1 20110407 - BOEHRINGER INGELHEIM INT [DE], et al
  • "View of NCT01002807 on 2009_10_26", CLINICALTRIALS.GOV ARCHIVE, 26 October 2009 (2009-10-26), XP002663638
  • V. KUKKAR ET AL.: "Mixing and formulation of low dose drugs: underlying problems and solutions", THAI J. PHARM. SCI., vol. 32, 2008, pages 43 - 58, XP055012249
  • M. PFISTER ET AL., CLINICAL PHARMACOLOGY & THERAPEUTICS, vol. 85, 5 May 2009 (2009-05-05), pages 513 - 519, XP009146835
  • "sodium glucose cotransport inhibition with dapagliflozin in type 2 diabes", DIABETES CARE, vol. 32, no. 4, April 2009 (2009-04-01), pages 650 - 657, XP055012106
  • U. MANDAL ET AL.: "Formulation and In Vitro Studies of a Fixed-Dose Combination of a Bilayer Matrix Tablet Containing Metformin HCl as Sustained Release and Glipizide as Immediate Release", DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, vol. 34, 2008, pages 305 - 313, XP055585729
  • J. CALADO: "Dapagliflozin, an oral sodium glucose cotransporter type 2 inhibitor for the treatment of type 2 diabetes mellitus", IDRUGS, vol. 12, no. 12, 2009, pages 785 - 798, XP009136677
  • TERRI L. ET AL: "NEW DRUGS IN DEVELOPMENT FOR THE THE TREATMENT OF DIABETES", DIABETES SPECTRUM, vol. 22, no. 2, 2009, pages 92 - 106, XP009123031
  • "Fixed-dose single tablet antidiabetic combinations", DIABETES , OBESITY AND METABOLISM, vol. 11, 2009, pages 527 - 533, XP055588773
  • DEBRA S. HAUSMAN: "COMPARISON OF LOW SHEAR, HIGH SHEAR, AND FLUID BED GRANULATION DURING LOW DOSE TABLET PROCESS DEVELOPMENT", DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY@, vol. 30, no. 3, 2004, pages 259 - 266, XP009050681
  • HANDBOOK OF PHARMACEUTICAL EXCIPIENTS, SIXTH ED., 5 February 2009 (2009-02-05), pages 129 - 133
  • JACK ZHENG, FORMULATION AND ANALYTICAL DEVELOPMENT FOR LOW-DOSE ORAL DRUG PRODUCTS, 2009, pages 63,77-78,86

Opponent : STADA Arzneimittel AG

Designated contracting state (EPC)

AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

DOCDB simple family (publication)

WO 2011060290 A2 20110519; WO 2011060290 A3 20120223; WO 2011060290 A8 20120712; AU 2010319377 A1 20120705; AU 2010319377 B2 20141023; BR 112012011733 A2 20190924; CA 2780941 A1 20110519; CA 2780941 C 20180612; CA 3002948 A1 20110519; CA 3002948 C 20201027; CN 102740839 A 20121017; CN 102740839 B 20150506; CN 104825417 A 20150812; CY 1121107 T1 20191211; DK 2498759 T3 20181126; EP 2498759 A2 20120919; EP 2498759 B1 20180801; ES 2693686 T3 20181213; HR P20181755 T1 20181228; JP 2013510875 A 20130328; JP 2015129142 A 20150716; JP 5784623 B2 20150924; LT 2498759 T 20181126; MX 2012005365 A 20120529; PL 2498759 T3 20190329; PT 2498759 T 20181115; RS 57926 B1 20190131; RU 2012124238 A 20131220; RU 2015122253 A 20181220; RU 2558798 C2 20150810; SI 2498759 T1 20181231; TR 201816242 T4 20181121; US 2013034606 A1 20130207; US 8871264 B2 20141028

DOCDB simple family (application)

US 2010056577 W 20101112; AU 2010319377 A 20101112; BR 112012011733 A 20101112; CA 2780941 A 20101112; CA 3002948 A 20101112; CN 201080061412 A 20101112; CN 201510185377 A 20101112; CY 181101139 T 20181101; DK 10782116 T 20101112; EP 10782116 A 20101112; ES 10782116 T 20101112; HR P20181755 T 20181024; JP 2012539026 A 20101112; JP 2015019631 A 20150203; LT 10782116 T 20101112; MX 2012005365 A 20101112; PL 10782116 T 20101112; PT 10782116 T 20101112; RS P20181289 A 20101112; RU 2012124238 A 20101112; RU 2015122253 A 20101112; SI 201031791 T 20101112; TR 201816242 T 20101112; US 201013509213 A 20101112